The purpose of this study is to investigate the tolerability, pharmacokinetic profile of BIA 3-202 and its metabolites, and the pharmacokinetic and pharmacodynamic interaction between 4 different single doses of BIA 3-202 (50 mg, 100 mg, 200 mg and 400 mg) and a single dose of standard levodopa 100 mg/benserazide 25 mg (Madopar® 125) in adult male and female healthy volunteers.
This was a single centre, double-blind, randomised, placebo-controlled, single-graded-dose, crossover study with five single-dose treatment periods. The washout period between doses was 15±2 days. For each of the five treatment periods, volunteers were to be admitted at the UFH on the day before the treatment day. On each treatment period, the pre-dose assessment were to be completed, BIA 3-202/Placebo was to be administered concomitantly with the dose of Madopar® 125 and post-dose assessments were to be completed. Subjects were discharged 30 h post-dose. Subjects should attend five treatment periods and were to receive a different dose of BIA 3-202 or placebo during each of these treatment periods.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
18
The study consisted of 5 treatment periods. Eligible subjects were admitted to the UFH on the morning of the day prior to receive the trial medication (dosing day) and remained in the unit for at least 30 h post-dose. Subjects were to receive BIA 3-202 50 mg, 100 mg, 200 mg, 400 mg and placebo at 5 separate treatment periods.
Placebo dose consisted of 5 tablets matching BIA 3-202 100 mg tablets; oral route.
Levodopa 100 mg/benserazide 25 mg capsules (Madopar® 125, marketed by Roche products Limited); oral route.
Human Pharmacology Unit - BIAL - Portela & Ca, S.A.
S. Mamede Do Coronado, S. Mamede Do Coronado, Portugal
Maximum observed plasma concentration (Cmax)
Time frame: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18 and 24 h post-dose
Area under the plasma concentration time curve extrapolated to infinity (AUC0-∞)
Time frame: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18 and 24 h post-dose
Apparent terminal elimination half-life (t1/2)
Time frame: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 18 and 24 h post-dose
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